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    • 4. 发明授权
    • p-Hydroxy phenone derivatives and the use thereof
    • P-羟基苯酮衍生物及其用途
    • US5118682A
    • 1992-06-02
    • US378966
    • 1989-07-12
    • Wilfried LubischManfred RaschackGerda von Philipsborn
    • Wilfried LubischManfred RaschackGerda von Philipsborn
    • A61K31/135A61K31/40A61K31/445A61P9/06C07C217/22C07D295/08C07D295/092
    • C07D295/088C07C217/22
    • p-Hydroxy phenone derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are identical or different and are methyl, chlorine, bromine and hydrogen, but R.sup.1, R.sup.2 and R.sup.3 are not all H,R.sup.4 and R.sup.5 are identical or different and are H, C.sub.1 -C.sub.4 -alkyl, or OR.sup.6, but R.sup.4 and R.sup.5 are not both H,X is a --CH.dbd.CH--, --CH.sub.2 CH.sub.2 or --CH.sub.2 -- bridge,Y is a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.4 bridge, andZ is NR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 are, independently of one another, hydrogen or C.sub.1-4 -alkyl, or Z is a 5- or 6-membered ring with a nitrogen atom in the 1 position and, where appropriate, additionally a second N atom or an O or S atom, the second N atom being substituted by R.sup.7, as well as the physiologically tolerated salts thereof,are used to prepare drugs antiarrhythmic of Vaughan-Williams class III.
    • 通式I的对羟基苯酮衍生物其中R 1,R 2和R 3相同或不同,为甲基,氯,溴和氢,但R 1,R 2和R 3不全为H,R 4和R 5相同 或不同的是H,C 1 -C 4烷基或OR 6,但R 4和R 5不同时为H,X为-CH = CH-,-CH 2 CH 2或-CH 2 - 桥,Y为直链或支链, 饱和或不饱和的C 1 -C 4桥,Z为NR 6 R 7,其中R 6和R 7彼此独立地为氢或C 1-4 - 烷基,或Z为在1位上具有氮原子的5-或6-元环 位置,并且在适当的情况下另外还有第二个N原子或O或S原子,被R7取代的第二个N原子及其生理上耐受的盐用于制备Vaughan-Williams III类抗心律不齐药物。
    • 10. 发明授权
    • Tetracyclic quinazoline derivatives, effective as antiarrythmic agents
    • 作为抗菌药物有效的四环喹诺酮衍生物
    • US5214047A
    • 1993-05-25
    • US243469
    • 1988-09-12
    • Bernd OstersehltRainer SchleckerBeatrice RendenbachGerda von PhilipsbornAlbrecht Franke, deceased
    • Bernd OstersehltRainer SchleckerBeatrice RendenbachGerda von PhilipsbornAlbrecht Franke, deceased
    • A61K31/505A61P9/06C07D471/14C07D487/14
    • C07D471/14C07D487/14
    • A tetracyclic quinazoline derivative of the formula I: ##STR1## wherein A is C.sub.2-3 -alkylene or C.sub.2-3 -alkylene which is substituted by one or two C.sub.1-4 -alkyl radicals or A is cyclohexylene; X is phenyl, naphthyl or phenyl or naphthyl which is substituted by halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.1 R.sup.2, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 -alkyl; or X is thienyl or thienyl which is substituted by chlorine, fluorine, methyl, ethyl, methoxy, ethoxy, nitro or hydroxyl; and R is hydrogen, halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.3 R.sup.4, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 -alkyl, and the pharmaceutically acceptable salts thereof. The compounds and compositions of the present invention are effective as antiarrhythmic agents.
    • 式I的四环喹唑啉衍生物:其中A是被一个或两个C 1-4 - 烷基取代的C 2-3亚烷基或C 2-3亚烷基,或者A是亚环己基; X是被卤素,硝基,氨基,C 1-4 - 烷基氨基,磺酰基氨基,C 1-4 - 酰氨基,羟基,C 1-4 - 烷氧基,-O-(CH 2)2-4取代的苯基,萘基或苯基或萘基 -NR 1 R 2,C 1-4 - 烷基或C 1-4 - 烷基磺酰基,其中R 1和R 2各自为氢或C 1-4 - 烷基; 或X是被氯,氟,甲基,乙基,甲氧基,乙氧基,硝基或羟基取代的噻吩基或噻吩基; 并且R是氢,卤素,硝基,氨基,C 1-4 - 烷基氨基,磺酰基氨基,C 1-4 - 酰氨基,羟基,C 1-4 - 烷氧基,-O-(CH 2)2-4 -NR 3 R 4,C 1-4 - 烷基 或C 1-4 - 烷基磺酰基,其中R 3和R 4各自为氢或C 1-4 - 烷基,及其药学上可接受的盐。 本发明的化合物和组合物作为抗心律失常药有效。